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Chemical Structure : LY3410738
Catalog No.: PC-49659Not For Human Use, Lab Use Only.
LY3410738 (LY 3410738) is a potent, selective, and covalent inhibitor of mutant IDH1 (IDH1-R132), LY3410738 is more effective than Ivosidenib (Cat#PC-45550) and potentiates antileukemic activity of AML.
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LY3410738 (LY 3410738) is a potent, selective, and covalent inhibitor of mutant IDH1 (IDH1-R132), LY3410738 is more effective than Ivosidenib (Cat#PC-45550) and potentiates antileukemic activity of AML.
LY3410738 modifies a single cysteine (Cys269) in an allosteric binding pocket and rapidly inactivates the enzyme, selectively inhibiting 2-HG production without affecting alpha-ketoglutarate (a-KG) levels.
LY3410738 displayed greater potency for inhibition of 2-HG production and differentiation of the IDH1 mutant cells compared to AG-120.
LY3410738 treatement caused sustained 2-HG inhibition leading to a more robust and durable efficacy with respect to AG-120 in vivo.
LY3410738 increased efficacy with Cytarabine and Azacitidine or the FLT3 inhibitor Midostaurin, exhibited a potent anti-leukemic effect, reduction of 2-HG level, and enhanced differentiation of the leukemic blasts in FLT3-mutated AML mice.
LY3410738 also showed synergistic effect when combined with FDA approved Bcl-2 inhibitor, venetoclax in isogenic cells with IDH1R132H mutation, as well as in AML xenograft model derived from a patient refractory to AG-120.
| M.Wt | 504.64 | |
| Formula | C28H36N6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Abstract 6417: Cancer Res (2020) 80 (16_Supplement): 6417.
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